Transporter

IC50 (mM)

Probe Substrate

Remogliflozin Etabonate

Remogliflozin

GSK279782

GSK333081

Pgp

>100

>100

>100

>100

[3H]-digoxin

OATP1B1

5.3 (1.1)a

25 (2.3)

14 (1.5)

NT

[3H]-estradiol 17β-D-glucuronide

OCT1

43.4 (3.7)

38.6 (1.6)

>100

>100

[14C]-tetraethylammonium

OCT3

>100

>100

>100

>100

[3H]-histamine

aData are the mean (± standard deviation) from triplicate wells.
NT: Not Tested
Table 1: Inhibition of Human ABC and SLC Transporters by Remogliflozin etabonate, Remogliflozin and Metabolites.